Characteristics of the substance Prometazine
Phenothiazine derivative. Crystalline powder of white or delicate yellow colour, odourless. Slowly oxidizes in the air, gaining a blue colour. Very easily soluble in water, well soluble in alcohol.
Pharmacological action – antiallergic, mesoanesthetic, antihistamine, antipruritic, anti-emetic, sedative.
Competitively blocks H1-histamine receptors, has antiexudative, anti-allergic, anti-inflammatory, mestnoanesthetic effect. Reduces capillary permeability, swelling of the mucous membranes, itching. Has adrenolytic, moderate peripheral and central cholinolytic action. Inhibits histamine-N-methyltransferase, blocks the central histamine H3-receptors. Suppresses the CNS, has a sedative, anxiolytic, antipsychotic and sleeping pills effect, lowers body temperature. Reduces the excitability of vestibular receptors, depresses the function of the labyrinth, eliminates dizziness. Antiemetizing effect due to blockage of the receptors of the chemoreceptor zone of the elongated brain. It penetrates through GB. If administered 2 weeks before delivery, it may depress platelet aggregation in newborns. In experimental studies, no mutagenic effect and adverse effects on fetal development were found.
It is quickly and completely absorbed from the GIT. During ingestion the effects appear after 15-60 min, at w / i – after 20 min, at w / i – after 3-5 min. Duration of action – 4-6 hours (after ingestion – up to 12 hours). It is associated with plasma proteins by 65-90%. Metabolized in the liver and partially in the kidneys, with the formation of sulfides prometazine, N-demethylprometazine and other derivatives. T1/2 – 7-14 hours. It is derived mainly from urine, including in the form of metabolites.
Use of the substance Prometazine
Allergodermatosis, pruritus, eczema, exudative diathesis, hives, rashes and other skin allergic reactions to drugs and chemicals, itching, allergic conjunctivitis, allergic rhinitis, pollinosis, stings of wasps, bees, scorpions, bumblebee, serum disease, angioedema, false cereals, asthmatic bronchitis, atopic bronchial asthma, anaphylactic and anaphylactoid reactions (as part of complex therapy), rheumatism with a pronounced allergic component; Meniere’s syndrome, dizziness, nausea and vomiting, sickness syndrome; anxiety, neuroses and neurosis-like conditions, psychosis, insomnia, extrapyramid disorders (against the background of neuroleptics), trigeminal neuralgia, migraine, chorea, hyperthermia; premedication and postoperative period (as a sedative, for artificial hibernation, potentiation of anesthesia and local anesthesia), study of gastric secretion (when used as a stimulant for histamine secretion).
Contraindications . Promethazine Dosage
Hypersensitivity (including to other phenothiazines), comatose state, simultaneous use of MAO inhibitors and a period of 14 days after their administration, alcohol intoxication, liver and/or kidney failure, pregnancy, lactation, occasional vomiting in children of unspecified genesis, early childhood up to 2 months (for parenteral administration), children under 6 years old (for ingestion). https://pillintrip.com/medicine/promethazin-neuraxpharm
Restrictions on use
Jaundice, prostate hypertrophy, predisposition to urinary retention, bladder neck stenosis, open- or closed-angle glaucoma, peptic ulcer with pyloroduodenal obstruction, lower respiratory tract diseases, oppression of bone marrow function, diseases of the cardiovascular system (severe angina, arterial hypertension, decompensated chronic heart failure, tachyarrhythmia), epilepsy, sleep apnea syndrome, Reye’s syndrome, pregnancy, breast-feeding, old age.
Application during pregnancy and breastfeeding
It’s contraindicated for pregnancy.
Category of action on the fetus by FDA.
Breastfeeding should be stopped for the duration of treatment.